Bile-acid-activated receptors: targeting TGR5 and farnesoid-X-receptor in lipid and glucose disorders.
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S. Fiorucci | G. Palladino | A. Mencarelli | Stefano Fiorucci | S. Cipriani | Sabrina Cipriani | Andrea Mencarelli | Giuseppe Palladino
[1] W. Mckeehan,et al. Independent Repression of Bile Acid Synthesis and Activation of c-Jun N-terminal Kinase (JNK) by Activated Hepatocyte Fibroblast Growth Factor Receptor 4 (FGFR4) and Bile Acids* , 2005, Journal of Biological Chemistry.
[2] R. Savkur,et al. Regulation of carbohydrate metabolism by the farnesoid X receptor. , 2005, Endocrinology.
[3] Shawn P Williams,et al. Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. , 2008, Bioorganic & medicinal chemistry letters.
[4] S. Kliewer,et al. Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis. , 2005, Cell metabolism.
[5] B. Staels,et al. Glucose regulates the expression of the farnesoid X receptor in liver. , 2004, Diabetes.
[6] J. Auwerx,et al. The small heterodimer partner interacts with the liver X receptor alpha and represses its transcriptional activity. , 2002, Molecular endocrinology.
[7] J. W. Becker,et al. Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation , 2008, Proceedings of the National Academy of Sciences.
[8] J. Hardies,et al. A placebo-controlled trial of pioglitazone in subjects with nonalcoholic steatohepatitis. , 2006, The New England journal of medicine.
[9] Darrell R. Abernethy,et al. International Union of Pharmacology: Approaches to the Nomenclature of Voltage-Gated Ion Channels , 2003, Pharmacological Reviews.
[10] G. Gwak,et al. Bile acid-induced TGR5-dependent c-Jun-N terminal kinase activation leads to enhanced caspase 8 activation in hepatocytes. , 2007, Biochemical and biophysical research communications.
[11] H. Davis,et al. Targeted deletion of Gpbar1 protects mice from cholesterol gallstone formation. , 2006, The Biochemical journal.
[12] S. Kliewer,et al. Differential regulation of bile acid homeostasis by the farnesoid X receptor in liver and intestine Published, JLR Papers in Press, August 24, 2007. , 2007, Journal of Lipid Research.
[13] K. Houck,et al. T0901317 is a dual LXR/FXR agonist. , 2004, Molecular genetics and metabolism.
[14] Min-Bo Chen,et al. 3D-QSAR studies with the aid of molecular docking for a series of non-steroidal FXR agonists. , 2007, Bioorganic & medicinal chemistry letters.
[15] B. Bouscarel,et al. Bile acids and signal transduction: role in glucose homeostasis. , 2008, Cellular signalling.
[16] Jasmine Chen,et al. Identification of Gene-selective Modulators of the Bile Acid Receptor FXR* , 2003, The Journal of Biological Chemistry.
[17] L. Moore,et al. Identification of a chemical tool for the orphan nuclear receptor FXR. , 2000, Journal of medicinal chemistry.
[18] Gabriele Costantino,et al. Farnesoid X receptor: from structure to potential clinical applications. , 2005, Journal of medicinal chemistry.
[19] D. Mangelsdorf,et al. A Natural Product That Lowers Cholesterol As an Antagonist Ligand for FXR , 2002, Science.
[20] J. Auwerx,et al. Bile acids and the membrane bile acid receptor TGR5--connecting nutrition and metabolism. , 2008, Thyroid : official journal of the American Thyroid Association.
[21] E. Distrutti,et al. Antiatherosclerotic effect of farnesoid X receptor. , 2009, American journal of physiology. Heart and circulatory physiology.
[22] Masataka Harada,et al. A G Protein-coupled Receptor Responsive to Bile Acids* , 2003, The Journal of Biological Chemistry.
[23] A. Fukamizu,et al. Bile Acids Regulate Gluconeogenic Gene Expression via Small Heterodimer Partner-mediated Repression of Hepatocyte Nuclear Factor 4 and Foxo1* , 2004, Journal of Biological Chemistry.
[24] P. Edwards,et al. Peroxisome proliferator-activated receptor-γ coactivator 1α (PGC-1α) regulates triglyceride metabolism by activation of the nuclear receptor FXR , 2004 .
[25] Yanqiao Zhang,et al. FXR, a multipurpose nuclear receptor. , 2006, Trends in biochemical sciences.
[26] C. Liddle,et al. Feed-forward Regulation of Bile Acid Detoxification by CYP3A4 , 2004, Journal of Biological Chemistry.
[27] P. Edwards,et al. FXR Deficiency Causes Reduced Atherosclerosis in Ldlr−/− Mice , 2006, Arteriosclerosis, thrombosis, and vascular biology.
[28] J. Auwerx,et al. Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5. , 2007, Journal of medicinal chemistry.
[29] B. Staels,et al. Role of bile acids and bile acid receptors in metabolic regulation. , 2009, Physiological reviews.
[30] Timothy M Willson,et al. Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice. , 2006, Proceedings of the National Academy of Sciences of the United States of America.
[31] K. Houck,et al. The Hypolipidemic Natural Product Guggulsterone Is a Promiscuous Steroid Receptor Ligand , 2005, Molecular Pharmacology.
[32] S. Wright,et al. Guggulsterone Is a Farnesoid X Receptor Antagonist in Coactivator Association Assays but Acts to Enhance Transcription of Bile Salt Export Pump* , 2003, The Journal of Biological Chemistry.
[33] A. Tiwari,et al. TGR5: an emerging bile acid G-protein-coupled receptor target for the potential treatment of metabolic disorders. , 2009, Drug discovery today.
[34] G. Reaven. Role of Insulin Resistance in Human Disease , 1988, Diabetes.
[35] Takao Nakamura,et al. Identification of membrane-type receptor for bile acids (M-BAR). , 2002, Biochemical and biophysical research communications.
[36] Wen Xie,et al. International Union of Pharmacology. LXII. The NR1H and NR1I Receptors: Constitutive Androstane Receptor, Pregnene X Receptor, Farnesoid X Receptor α, Farnesoid X Receptor β, Liver X Receptor α, Liver X Receptor β, and Vitamin D Receptor , 2006, Pharmacological Reviews.
[37] H. Miyoshi,et al. Targeted disruption of G protein-coupled bile acid receptor 1 (Gpbar1/M-Bar) in mice. , 2006, The Journal of endocrinology.
[38] D. Häussinger,et al. Expression and function of the bile acid receptor TGR5 in Kupffer cells. , 2008, Biochemical and biophysical research communications.
[39] J. Auwerx,et al. Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. , 2008, Journal of medicinal chemistry.
[40] Grace Guo,et al. The Farnesoid X-receptor Is an Essential Regulator of Cholesterol Homeostasis* , 2003, The Journal of Biological Chemistry.
[41] E. Distrutti,et al. Targeting farnesoid X receptor for liver and metabolic disorders. , 2007, Trends in molecular medicine.
[42] C. Huard,et al. A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia. , 2009, American journal of physiology. Gastrointestinal and liver physiology.
[43] S. Kliewer,et al. FXR agonists and FGF15 reduce fecal bile acid excretion in a mouse model of bile acid malabsorption Published, JLR Papers in Press, September 6, 2007. , 2007, Journal of Lipid Research.
[44] J. Chiang,et al. Bile acids: regulation of synthesis , 2009, Journal of Lipid Research.
[45] P. Dawson,et al. OSTα‐OSTβ: A major basolateral bile acid and steroid transporter in human intestinal, renal, and biliary epithelia , 2005 .
[46] J. Orava,et al. Functional brown adipose tissue in healthy adults. , 2009, The New England journal of medicine.
[47] D. Drucker,et al. Biology of incretins: GLP-1 and GIP. , 2007, Gastroenterology.
[48] G. Casari,et al. Identification of Farnesoid X Receptor β as a Novel Mammalian Nuclear Receptor Sensing Lanosterol , 2003, Molecular and Cellular Biology.
[49] C. J. Sinal,et al. Loss of functional farnesoid X receptor increases atherosclerotic lesions in apolipoprotein E-deficient mice Published, JLR Papers in Press, September 26, 2005. DOI 10.1194/jlr.M500390-JLR200 , 2005, Journal of Lipid Research.
[50] Roberto Pellicciari,et al. Structural basis for bile acid binding and activation of the nuclear receptor FXR. , 2003, Molecular cell.
[51] Antonio Macchiarulo,et al. Molecular Field Analysis and 3D-Quantitative Structure-Activity Relationship Study (MFA 3D-QSAR) Unveil Novel Features of Bile Acid Recognition at TGR5 , 2008, J. Chem. Inf. Model..
[52] D. Russell,et al. Loss of nuclear receptor SHP impairs but does not eliminate negative feedback regulation of bile acid synthesis. , 2002, Developmental cell.
[53] T. Willson,et al. Farnesoid X-activated receptor induces apolipoprotein C-II transcription: a molecular mechanism linking plasma triglyceride levels to bile acids. , 2001, Molecular endocrinology.
[54] J. Dallongeville,et al. Bile acid-activated nuclear receptor FXR suppresses apolipoprotein A-I transcription via a negative FXR response element. , 2002, The Journal of clinical investigation.
[55] C. Lavie,et al. Obesity and cardiovascular disease: risk factor, paradox, and impact of weight loss. , 2009, Journal of the American College of Cardiology.
[56] J. Auwerx,et al. Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation , 2006, Nature.
[57] Shufeng Zhou,et al. Multidrug resistance associated proteins as determining factors of pharmacokinetics and pharmacodynamics of drugs. , 2007, Current drug metabolism.
[58] T. A. Kerr,et al. Molecular basis for feedback regulation of bile acid synthesis by nuclear receptors. , 2000, Molecular cell.
[59] J. Auwerx,et al. Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea. , 2007, Biochemical and biophysical research communications.
[60] F. Lammert,et al. Functional variants of the central bile acid sensor FXR identified in intrahepatic cholestasis of pregnancy. , 2007, Gastroenterology.
[61] Kazuhide Inoue,et al. The novel compounds that activate farnesoid X receptor: the diversity of their effects on gene expression. , 2008, Journal of pharmacological sciences.
[62] M. Makishima,et al. The orphan nuclear receptor, shp, mediates bile acid-induced inhibition of the rat bile acid transporter, ntcp. , 2001, Gastroenterology.
[63] G. Tsujimoto,et al. Bile acids promote glucagon-like peptide-1 secretion through TGR5 in a murine enteroendocrine cell line STC-1. , 2005, Biochemical and biophysical research communications.
[64] Folkert Kuipers,et al. The Farnesoid X Receptor Modulates Adiposity and Peripheral Insulin Sensitivity in Mice* , 2006, Journal of Biological Chemistry.
[65] Wooin Lee,et al. A common polymorphism in the bile acid receptor farnesoid X receptor is associated with decreased hepatic target gene expression. , 2007, Molecular endocrinology.
[66] F. Baldelli,et al. Farnesoid X receptor agonists in biliary tract disease , 2009, Current opinion in gastroenterology.
[67] M. Evans,et al. Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR−/− and apoE−/− mice Published, JLR Papers in Press, January 27, 2009. , 2009, Journal of Lipid Research.
[68] M. Bowman,et al. A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. , 2003, Molecular cell.
[69] D. Russell. The enzymes, regulation, and genetics of bile acid synthesis. , 2003, Annual review of biochemistry.
[70] T. Osborne,et al. FGF15/FGFR4 Integrates Growth Factor Signaling with Hepatic Bile Acid Metabolism and Insulin Action* , 2009, Journal of Biological Chemistry.
[71] Masahiro Tohkin,et al. Targeted Disruption of the Nuclear Receptor FXR/BAR Impairs Bile Acid and Lipid Homeostasis , 2000, Cell.
[72] Sander M Houten,et al. Bile acids lower triglyceride levels via a pathway involving FXR, SHP, and SREBP-1c. , 2004, The Journal of clinical investigation.
[73] G. Farrell,et al. Nonalcoholic fatty liver disease: From steatosis to cirrhosis , 2006, Hepatology.
[74] T. Willson,et al. Protective Effects of 6-Ethyl Chenodeoxycholic Acid, a Farnesoid X Receptor Ligand, in Estrogen-Induced Cholestasis , 2005, Journal of Pharmacology and Experimental Therapeutics.
[75] M. Trauner,et al. Role of nuclear receptors in the adaptive response to bile acids and cholestasis: pathogenetic and therapeutic considerations. , 2006, Molecular pharmaceutics.
[76] L. Moore,et al. A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis. , 2000, Molecular cell.
[77] D. Häussinger,et al. The G‐protein coupled bile salt receptor TGR5 is expressed in liver sinusoidal endothelial cells , 2007, Hepatology.
[78] Folkert Kuipers,et al. The Farnesoid X Receptor Modulates Hepatic Carbohydrate Metabolism during the Fasting-Refeeding Transition* , 2005, Journal of Biological Chemistry.
[79] Songwen Zhang,et al. Farnesoid X receptor agonist WAY-362450 attenuates liver inflammation and fibrosis in murine model of non-alcoholic steatohepatitis. , 2009, Journal of hepatology.
[80] S. Ito,et al. Activation of Nuclear Factor (Erythroid-2 Like) Factor 2 by Toxic Bile Acids Provokes Adaptive Defense Responses to Enhance Cell Survival at the Emergence of Oxidative Stress , 2007, Molecular Pharmacology.
[81] T. Willson,et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. , 2002, Journal of medicinal chemistry.
[82] Ke Ma,et al. Farnesoid X receptor is essential for normal glucose homeostasis. , 2006, The Journal of clinical investigation.
[83] Johan Auwerx,et al. Targeting bile-acid signalling for metabolic diseases , 2008, Nature Reviews Drug Discovery.